Department of Biotechnology, Institute of Biotechnology, Life and Applied Sciences, Yeungnam University, Gyeongsan 38541, Korea.
Department of Biology, College of Natural Sciences, Kyungpook National University, Buk-gu, Daegu 41566, Korea.
Molecules. 2022 Nov 1;27(21):7432. doi: 10.3390/molecules27217432.
Quercetin (Qu) is a dietary antioxidant and a member of flavonoids in the plant polyphenol family. Qu has a high ability to scavenge reactive oxygen species (ROS) and reactive nitrogen species (RNS) molecules; hence, exhibiting beneficial effects in preventing obesity, diabetes, cancer, cardiovascular diseases, and inflammation. However, quercetin has low bioavailability due to poor water solubility, low absorption, and rapid excretion from the body. To address these issues, the usage of Qu nanosuspensions can improve physical stability, solubility, and pharmacokinetics. Therefore, we developed a Qu and polyethylene glycol nanosuspension (Qu-PEG NS) and confirmed its interaction by Fourier transform infrared analysis. Qu-PEG NS did not show cytotoxicity to HaCaT and RAW 264.7 cells. Furthermore, Qu-PEG NS effectively reduced the nitrogen oxide (NO) production in lipopolysaccharide (LPS)-induced inflammatory RAW 264.7 cells. Additionally, Qu-PEG NS effectively lowered the levels of COX-2, NF-κB p65, and IL-1β in the LPS-induced inflammatory RAW 264.7 cells. Specifically, Qu-PEG NS exhibited anti-inflammatory properties by scavenging the ROS and RNS and mediated the inhibition of NF-κB signaling pathways. In addition, Qu-PEG NS had a high antioxidant effect and antibacterial activity against and . Therefore, the developed novel nanosuspension showed comparable antioxidant, anti-inflammatory, and antibacterial functions and may also improve solubility and physical stability compared to raw quercetin.
槲皮素(Qu)是一种膳食抗氧化剂,也是植物多酚类黄酮家族的成员。Qu 具有清除活性氧(ROS)和活性氮(RNS)分子的高能力;因此,在预防肥胖、糖尿病、癌症、心血管疾病和炎症方面具有有益作用。然而,由于槲皮素的水溶性差、吸收率低且在体内迅速排泄,因此其生物利用度较低。为了解决这些问题,使用 Qu 纳米混悬剂可以提高物理稳定性、溶解度和药代动力学。因此,我们开发了一种 Qu 和聚乙二醇纳米混悬剂(Qu-PEG NS),并通过傅里叶变换红外分析确认了它们的相互作用。Qu-PEG NS 对 HaCaT 和 RAW 264.7 细胞没有细胞毒性。此外,Qu-PEG NS 能有效抑制脂多糖(LPS)诱导的炎症 RAW 264.7 细胞中一氧化氮(NO)的产生。此外,Qu-PEG NS 能有效降低 LPS 诱导的炎症 RAW 264.7 细胞中 COX-2、NF-κB p65 和 IL-1β 的水平。具体来说,Qu-PEG NS 通过清除 ROS 和 RNS 发挥抗炎作用,并介导 NF-κB 信号通路的抑制。此外,Qu-PEG NS 对 和 具有高抗氧化作用和抗菌活性。因此,与槲皮素原药相比,开发的新型纳米混悬剂具有相当的抗氧化、抗炎和抗菌功能,并且可能还提高了溶解度和物理稳定性。